US5962493AExpiredUtility

2-mercaptobenzimidazole derivatives and antihyperlipemic agent or antiarteriosclerotic agent containing the same

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Assignee: FUJI PHOTO FILM CO LTDPriority: Feb 4, 1994Filed: Nov 21, 1997Granted: Oct 5, 1999
Est. expiryFeb 4, 2014(expired)· nominal 20-yr term from priority
A61K 31/4184A61P 3/06A61P 9/10C07D 235/28
30
PatentIndex Score
0
Cited by
21
References
10
Claims

Abstract

2-Mercaptobenzimidazole derivatives represented by the following formulae, analogs and salts thereof are disclosed: ##STR1## These 2-mercaptobenzimidazole derivatives are useful as a medicine such as an antihyperlipemic agent or antiarteriosclerotic agent and also useful as an additive for silver halide photosensitive materials, liquid crystals and the like.

Claims

exact text as granted — not AI-modified
What is claimed is: 
     
       1. A method for inhibiting hyperlipemia or atherosclerosis comprising administering an effective amount of a 2-mercaptobenzimidazole compound represented by formula IV: ##STR13## wherein R 3  and R 4  each represent a hydrogen atom, a halogen atom, or an alkyl, alkoxy, alkoxycarbonyl, carbamoyl, sulfamoyl, acylamino, sulfonylamino, cyano or nitro group; R 50  and R 60  each represent a hydrogen atom, alkyl group, or acyl group;   n 3 , n 4 , each represent 1 or 2; and   L 2  represents a connecting group which is an alkylene group or a phenylene group-containing an alkylene group, or   a pharmaceutically acceptable salt thereof, to a mammal.   
     
     
       2. The method of claim 1, wherein the 2-mercaptobenzimidazole compound is a compound represented by formula IV-a: ##STR14## wherein L 2 , R 50  and R 60  are as defined in claim 1, R 31  and R 32  are the same as R 3 , and R 41  and R 42  are the same as R 4 . 
     
     
       3. The method of claim 2, wherein R 31 , R 32 , R 41 , R 42 , R 50  and R 60  in formula IV-a are hydrogen, and L 2  is an alkylene group having 4 to 10 carbon atoms or an alkylene-phenylene-alkylene group wherein each alkylene moiety of the alkylene-phenylene-alkylene group has 1 to 2 carbon atoms. 
     
     
       4. The method of claim 2, wherein one of R 31  and R 32  and one of R 41  and R 42  in formula IV-a are hydrogen, and the other one of R 31  and R 32  and the other one of R 41  and R 42  are lower alkyl, halogen, nitro or lower acylamino, and R 50  and R 60  are hydrogen, lower alkyl or lower alkanoyl. 
     
     
       5. The method of claim 2, wherein R 31 , R 32 , R 41  and R 42  in formula IV-a are halogen, and R 50  and R 60  are hydrogen. 
     
     
       6. The method of claim 2, wherein R 31 , R 32 , R 41  and R 42  in formula IV-a are hydrogen, and R 50  and R 60  are lower alkanoyl or lower alkyl, and L 2  is an alkylene group having 4 to 10 carbon atoms or an alkylene-phenylene-alkylene group, wherein each alkylene moiety of the alkylene-phenylene-alkylene group has 1 to 2 carbon atoms. 
     
     
       7. The method of claim 2, wherein R 31 , R 32 , R 41  and R 42  in formula IV-a are halogen or lower alkyl, and R 50  and R 60  are lower alkanoyl or lower alkyl. 
     
     
       8. A method for therapy of hyperlipemia or atherosclerosis in a mammal comprising administering an effective amount of a 2-mercaptobenzimidazole compound represented by formula IV: ##STR15## wherein R 3  and R 4  each represent a hydrogen atom, halogen atom, or alkyl, alkoxy, alkoxycarbonyl, carbamoyl, sulfamoyl, acylamino, sulfonylamino, cyano or nitro group; R 50  and R 60  each represent a hydrogen atom, alkyl group, or acyl group;   n 3 , n 4  each represent 1 or 2; and,   L 2  represents a connecting group which is an alkylene group or phenylene group-containing alkylene group, or   a pharmaceutically acceptable salt thereof, to a mammal.   
     
     
       9. A method for inhibiting foamy macrophages in a mammal comprising contacting a foamy macrophage with an effective amount of a 2-mercaptobenzimidazole compound represented by formula IV: ##STR16## wherein R 3  and R 4  each represent a hydrogen atom, a halogen atom, or an alkyl, alkoxy, alkoxycarbonyl, carbamoyl, sulfamoyl, acylamino, sulfonylamino, cyano or nitro group; R 50  and R 60  each represent a hydrogen atom, alkyl group, or acyl group;   n 3 , n 4  each represent 1 or 2; and   L 2  represents a connecting group which is an alkylene group or a phenylene group-containing an alkylene group, or   a pharmaceutically acceptable salt.   
     
     
       10. A method for reducing the formation of cholesteryl ester in foamy macrophages in a mammal comprising contacting a foamy macrophage with an effective amount of a 2-mercaptobenzimidazole compound represented by formula IV: ##STR17## wherein R 3  and R 4  each represent a hydrogen atom, a halogen atom, or an alkyl, alkoxy, alkoxycarbonyl, carbamoyl, sulfamoyl, acylamino, sulfonylamino, cyano or nitro group; R 50  and R 60  each represent a hydrogen atom, alkyl group, or acyl group;   n 3 , n 4  each represent 1 or 2; and   L 2  represents a connecting group which is an alkylene group or a phenylene group-containing an alkylene group, or   a pharmaceutically acceptable salt thereof.

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